Instruction for use: Zolmitriptan

The Latin name of the substance Zolmitriptan

Zolmitriptanum (genus. Zolmitriptani)

Chemical name

(4S) -4 - [[3- [2- (Dimethylamino) ethyl] -1H-indol-5-yl] methyl] -2-oxazolidinone

Gross formula

C₁₆H₂₁N₃O₂

Pharmacological group

Serotonergic agents

The nosological classification (ICD-10)

G43 Migraine: The pain of migraine; Migraine; hemiplegic migraine; Migraine headache; A migraine attack; Continuous headache; hemicranias

CAS Code

139264-17-8

Characteristics of the substance Zolmitriptan

White or almost white powder. Easily soluble in water. Molecular weight 287.36.

Pharmacology

Pharmacological action - antimigraine.

Selectively stimulates 5-HT1B / 1D serotonin receptors, has a moderate affinity for 5-HT1A receptors. It causes vasoconstriction, inhibits release of neuropeptides (vasoactive intestinal peptide, substance P and others.).

Well absorbed from the gastrointestinal tract, Cmax is reached within 1 h. Bioavailability is slightly more than 40% (the effect of "first passage" through the liver). Binding to plasma proteins is about 25%. T1 / 2 -. 2.5-3 h under intense liver biotransformation to form the N-desmethyl derivative (2-6 times more active than the starting material) and a number of inactive metabolites. It is excreted mainly by kidneys in the form of metabolites, about 30% - with feces in unchanged form.

Suspends the development of a migraine attack without direct analgesic action. In addition to stopping the attack of pain, it weakens nausea, vomiting (especially with left-side attacks), photo and phonophobia. The effect begins in 15-20 minutes and reaches a maximum within 1 hour. A greater effect is observed when taking at an altitude of an attack. It is highly effective in the complex treatment of migraine status (a series of several heavy, sequential migraine attacks lasting 2-5 days). Eliminates menstrual migraines. High doses have a sedative effect and cause drowsiness.

Application of substance Zolmitriptan

Migraine (arresting an attack).

Contraindications

Hypersensitivity, uncontrolled hypertension, ischemic heart disease, WPW-syndrome with cardiac arrhythmias, severe liver problems, children (under 18 years) and older (over 65) age.

Update of information

Contraindications (optional)

Hemiplegic, and oftalmoplegicheskaya basilar migraine, coronary vasospasm / Prinzmetal angina, peripheral artery disease, cerebrovascular disease (including stroke or transient ischemic attack), a history of severe renal failure (creatinine clearance less than 15 mL / min), co-application with other agonists of the 5-HT1B / 1D-serotonin receptors (e.g., sumatriptan, naratriptanom), ergotamine and its derivatives (including methysergide) and for 24 hours after their withdrawal; Joint application with MAO A inhibitors and within 14 days after their cancellation.

Application in pregnancy and lactation

Perhaps, if the expected effect of therapy exceeds the potential risk to the fetus.

The action category for fetus by FDA is C.

At the time of treatment should stop breastfeeding.

Side effects of Zolmitriptan

Nausea, dry mouth, dizziness, drowsiness, feeling of heat, fatigue, feeling of heaviness and constriction in the throat, neck, limbs and chest, a transient increase in blood pressure, myalgia, muscle weakness, paresthesia.

Interaction

Moclobemide increases the content in tissues.

Overdose

Symptoms: sedation.

Treatment: symptomatic therapy, incl. Ensuring airway patency, monitoring and maintaining the function of the cardiovascular system.

Routes of administration

Inside.

Precautions for the substance Zolmitriptan

Before the start of treatment, a detailed neurological examination is necessary to eliminate the organic pathology of the central nervous system, as well as assess the state of the cardiovascular system. It is not recommended to take concomitantly with other drugs from the group of 5-HT1D receptor agonists and use migraine attacks for prophylaxis.

Do not use during work drivers of vehicles and people whose profession is associated with increased concentration of attention.